Term
| what are the 4 main uses for estrogen or progesterone drugs |
|
Definition
hormone replacement therapy / post-menopause
contraception
health benifits of contraception
receptor antagonist: breast cancer, infertility |
|
|
Term
| what is another name for the follicular phase, how long is it |
|
Definition
| proliferative phase, length varies |
|
|
Term
| what are the two phases of the menstural cycle |
|
Definition
|
|
Term
| what is another name for the lutela phase, how long is it |
|
Definition
|
|
Term
| explain the process of hormone production in the follicular phase |
|
Definition
pulses of GnRH cause release of LH and FSH
estrogen increases reduce LH and FSH release
inhibin is mad ein ovary and causes feedback decreasing FSH
mid cycle estrogen reaches peak for 36 hours and stops inhibiting gonadotropins and causes surge instead |
|
|
Term
| what happens in the luteal phase |
|
Definition
corpus luteum secretes progesterone (estrgen levels stay elevated)
if pregnancy does not occur corpus luteum regresses due to lack of LH and progesterone and falls so endometrium sheds causing menstural discharge |
|
|
Term
| what does progesterone do for the baby/uterus |
|
Definition
stops endometrium proliferation
helps with implantation and growth of blastocyst
causes growth of endometrial vessels |
|
|
Term
| what is the general structure of estrogen |
|
Definition
| 18C with an aromatic phenolic acid ring (required for selective high affinity binding) |
|
|
Term
| what is the natural form of estrogen, where is it made in men and women |
|
Definition
17B estradiol
women: ovarian granulosa cells
men and post-menopause; adipose tissue viea DHEA from adrenal cortex |
|
|
Term
| what stimulates for estrogen release |
|
Definition
| gonadotropins stimulate aromatase |
|
|
Term
| what are precursors for estrogen |
|
Definition
androstendione
testosterone |
|
|
Term
| estrogen needs aromatic ring to work, how does it get it |
|
Definition
| aromatase using NADPH and O |
|
|
Term
| where are estrogen receptors located |
|
Definition
| ovarian granulosa, sertoli and leydig cells, stroma of adipose, placenta, blastocyte, brain |
|
|
Term
| how is estrogen converted between its different forms |
|
Definition
estradiol oxidized to esterone via 12-hydroxysteroid DH
estradiol and esterone converted to estriol |
|
|
Term
| what is the down side of using natural progesterone |
|
Definition
|
|
Term
| what are the two types of synthetic progesterone |
|
Definition
21C progesterone skeletons
19-nortestosterone |
|
|
Term
| what is 19-nortestosterone |
|
Definition
progesterone without C19, 20, 21
resembles testosterone more so has effects of both |
|
|
Term
| where is progesterone made, when |
|
Definition
made in testis, adrenal cortex, placenta, and ovary corpus luteum
begins being made in follicular phase and increases in luteal phase later in pregnancy |
|
|
Term
| what is the relationship between progesterone and the cns |
|
Definition
| increases body temp 1 deg midcycle until onset of menstural flow (ovulation) |
|
|
Term
| what is the down side to using estrogen alone in hormone replacement |
|
Definition
| risk of endometrial carcinoma due to hyperplasia of the endometrium |
|
|
Term
| what is the benifit of combined estrogen progesterone therapy in hormone replacement |
|
Definition
| estrogen receptors dont get out of hand because it has to make some progesterone receptors too |
|
|
Term
| how is a post-menopausal women with a uterus treated forr hormone replacement |
|
Definition
| progesterone/estrogen combination |
|
|
Term
| what are contraindications to progesterone/estrogen hormon replacement |
|
Definition
unable to tolerate progestins
risk of cardiovascular disease
poorlipoproteins use estrogen alone |
|
|
Term
| how is a post-menopausal women with a hysterctomy treated for homeone replacement |
|
Definition
| estrogen alone, no where for it to cause carcinoma |
|
|
Term
| what are 4 ways to administer hormone replacement therapy |
|
Definition
cyclic
continous
transdermal patch
vaginal ring |
|
|
Term
| what is the redigmen for cyclic hormone replacement |
|
Definition
estrogen 15d
estrogen and progesterone 10d
repeat |
|
|
Term
| what is the redigmen for continous hormone replacement |
|
Definition
estrogen and progesterone daily
OR
estrogen and progesterone 10d
esteogrn 15d
repeat |
|
|
Term
| what are the contents of combination oral contraceptives |
|
Definition
estrogen: ethinyl estradiol or mestraol
progesterone: norethindrone or norgestrel |
|
|
Term
| what are the three types of oral contraceptives |
|
Definition
monophasic
biphasic
triphasic |
|
|
Term
| how are monophasic oral contraceptives administered |
|
Definition
| same amount of estrogen and progesterone in each tablet for 21d |
|
|
Term
| how are biphasic oral contraceptives administred |
|
Definition
| two tablets with different amounts for 21 days |
|
|
Term
| what is the benifit of biphasic oral contraceptives |
|
Definition
| reduce steroids administred because it approximates estrogen to progesterin ratio of menstural cycle |
|
|
Term
| how are triphasic oral contraceptives administered |
|
Definition
| three tablets with different amounts for 21 days |
|
|
Term
| what is the general MOA of contraceptives |
|
Definition
estrogen supresses FSH and stops follicular development
proteitiating action of progestrin which stops LH surfe
progesterin stops ovulation, thickens cervical mucous, and causes endometrial atrophy
estrogen stabilizes endometrial lining (bleeding control) |
|
|
Term
| what are 4 contraindications to oral contraceptives |
|
Definition
thrombotic disease
over 35 and smoking
hormone sensitive tumor (breast canceR)
pregnancy |
|
|
Term
| what are the 4 forms of estrogen, talk about the bioavailability and blood distribution of each |
|
Definition
natural: 12B estradiol, esterone, estriol: poor oral bioavailability high first pass effect
17B estradiol estrace: microcrystaline form, reduced first pass |
|
|
Term
| what are the benifits of a transdermal estrogen patch |
|
Definition
slow release
increased bioavailability
constant blood levels |
|
|
Term
| what are the 4 types of synthetic estrogens |
|
Definition
conjugated
ethinyl estradiol
menastrol
estradiol cruptionate |
|
|
Term
| what is conjugated estrogen made of where does it come from |
|
Definition
many conjugated estrogen metabolites
pregnant mares |
|
|
Term
| what is the structure of ethinyl estradiol |
|
Definition
| ethinyl group on C17 of estrace nucleus |
|
|
Term
| how is mestranol metabolized |
|
Definition
prodrug
converted to ethinyl estradiol |
|
|
Term
| what is a non-steroidal estrogen agonist |
|
Definition
|
|
Term
| what is the MOA of oestrogen contraceptives |
|
Definition
passivly diffuse into cell
bind nuclear receptors in genital, breast, HPA, bone, and liver
interact with estrogen response elements (ERE) which alter transcription
supress FSH stopping follicle development and stabilizing endometrial lining (bleeding control) |
|
|
Term
| what are the 12 negative side effects of estrogen contraceptives |
|
Definition
elevated TG
decrease bile acid (due to cholesterol secretion)
removal: hot flashes, chills, sweating, parasthesia
nausea
cramping
fluid retention
dizzy
headache
breast tenderness
Mi or thrombosis in women >35 who smoke |
|
|
Term
| what are the good side effects of estrogen contraceptives (and natural functions) (14) |
|
Definition
decrease cholesterol
increase HDL
decrease LDL
growth of uterus, vagina, fallopian tubes, breast, ducts, sexual development
fat distribution, growth spurt, fusion of epiphysis
increase plasma binding proteins
prevent bone loss: block reabsorption
decrease endometrial and ovarian cancer
decrease fibroadenomas, fibrocysts, PID
decrease blood loss and cause cycle regularity |
|
|
Term
| why are esgtrogen contraceptives used (7) |
|
Definition
contraception
replacement
fibroadenomas
fibrocysts
PID
cycle regularity
failure of ovarian development |
|
|
Term
| what are three diseases that include failure of ovarian development |
|
Definition
dwarfism
turner syndrome
hypopituitarism |
|
|
Term
| what is the administration of the 4 estrogen contraceptives |
|
Definition
conjugated: oral active
ethinyl estradiol: oral active
mestranol: not for replacement
estradiol crypionate: long acting given IM |
|
|
Term
| how are estrogen drugs excreted |
|
Definition
| in urine with glucourindes and sulfate conjugates |
|
|
Term
| what are the side effects of diethylstilbesterol |
|
Definition
| congenital abnormalities in fetus |
|
|
Term
| why would you use diethylstilbesterol |
|
Definition
|
|
Term
| what are the three antiestrogen drugs |
|
Definition
chlomiphene
tamoxifen
raloxifene |
|
|
Term
|
Definition
competitive agonist of estrogen binding
stimulates ovulation in women with normal HPA and estrogen levels by opposing negative feedback increasing gonadotropin pulse amplitude (not frequency) |
|
|
Term
|
Definition
competitive antagonist of estrogen binding
antagonizes receptor |
|
|
Term
|
Definition
partial agonist effect on bone reabsorption and plasma lipoproteins
NO effect on reproductive tissues
selective estrogen receptor modulator |
|
|
Term
| what is the structure of clomiphene |
|
Definition
mixed isomeres
cis has estrogenic activity
trans has anti-estrogenic activity |
|
|
Term
| what is the structure of tamoxifen |
|
Definition
| pure trans isomere (only the useful part of clomiphene) |
|
|
Term
| why would you use clomiphene |
|
Definition
|
|
Term
| why would you use tamoxifen |
|
Definition
block hormone induced breast tumors
adjunct with surgery or chemo |
|
|
Term
| why would you use raloxifene |
|
Definition
| osteoperosis post-menopause |
|
|
Term
| what are the side effects of clomiphene (6 |
|
Definition
ovarian hyperstimulation
increased multiple births
ovarian cysts
anti-estrogenic: follicle, endometrium, cervical mucous (counter active) |
|
|
Term
| what are the side effects of tamoxifen (3) |
|
Definition
decrease tumor development in other breast
endometrial carcinoma
hormone independent breast tumors |
|
|
Term
| how is clomiphene administered, half life, where metabolized, where excreted |
|
Definition
oral
t.5 = 5-7d
hepatic metabolism
GI excretion |
|
|
Term
| tamoxifen: aministration, metabolism, excretion |
|
Definition
oral
hepatic metabolism
Gi excretion |
|
|
Term
| explain how tamoxifen is eliminated |
|
Definition
phase 1: 4-11d
phase 2: 4d (hydroxytamoxifen) |
|
|
Term
| what are the two aromatase modifying drugs |
|
Definition
|
|
Term
|
Definition
selective aromatase inhibitor stops conversion of androgens to estrogens
reversible |
|
|
Term
|
Definition
aromatase inactivastor acts as false substrate for enzyme and intermediate irreversibly binding to acrive site (suicide inhibition) stopping conversion of androgens to estrogens
irreversible |
|
|
Term
| what is the clinical use of amastrazole |
|
Definition
| post-menopausal hormone dependent breast cancer |
|
|
Term
| what is the use of exemestane |
|
Definition
| post-menopausal hormone dependent breast cancer |
|
|
Term
| what is an anti-progesterin drug, what progesterin structure family is it from |
|
Definition
mifepristone
19-nortestosterone derivative |
|
|
Term
|
Definition
potent competitive inhibitor of progesterone and glucocorticoids
decrease in progesterone cause abortion by detaching blastocyst
myometrial contraction and cervical softening allow for expulsion |
|
|
Term
|
Definition
administer up until 49 days after pregnancy
abortion pill |
|
|
Term
| what are the 4 progesterone contraceptives and their progesterone structure family |
|
Definition
norethindrone: 19-nortestosterone
norgestrel: 19-nortestosterone
mexroxyprogesterone acetate: 21C progesterone
progestasert |
|
|
Term
| what is the admnistration of the 4 progesterone contraceptives |
|
Definition
norethindrone: oral
norgestrel: oral, subdermal (5y)
mexroxyprogesterone acetate: IM (3mo)
progestasert: intrauterine |
|
|
Term
| MOA progesterone contraceptives |
|
Definition
supresses LH surge
thickens cervical mucous
decreases endometrial proliferation
stops ovulation |
|
|
Term
| where are progesterone receptors |
|
Definition
| genital, mammary, CNS (hypothalamus) |
|
|
Term
| what is the role of progesterone in pregnancy |
|
Definition
maintains it
supresses mensturation and uterine contraction
proliferation of mammary acini |
|
|
Term
| why not use a progesterone contraceptive all alone |
|
Definition
|
|
Term
| what are the uses of progesterone contraceptives |
|
Definition
ovarian supression: dysmenorrhea, endometrosis, histurism, uterine bleeding
hormone replacement: combined with estrogen
fibroadenomas
fibrocysts
PID
cycle regulation |
|
|
Term
| in general why is progesterone added to estrogen contraceptives, why aernt progesterone side effects a big deal |
|
Definition
avoid side effects of estrogen
progesterone side effects usually go away after 1 year |
|
|
Term
| what are the side effects of progesterone contraceptives (11) |
|
Definition
spotting
amenorrhea
decreased HDL
increased LDL
edema
weight gain: fat deposition
bloating
acne
histuism
impaired glucose tolerance: longer term, short term increases basal insulin
MI and thrombosis in women >35 who smoke |
|
|
Term
| MOA of the morning after pill |
|
Definition
| combination oral contraceptive in a high dose |
|
|
Term
| administration of the morning after pill |
|
Definition
taken within 72 hours of intercourse
ineffective after 7 days (cannot un-implant) |
|
|
Term
| what is the 21 patch made of |
|
Definition
| ethinyl estradiol norelgestromin |
|
|
Term
| administration of 21 patch |
|
Definition
|
|
Term
|
Definition
|
|
